ECSP13012543A - Análogos de buprenorfina - Google Patents
Análogos de buprenorfinaInfo
- Publication number
- ECSP13012543A ECSP13012543A ECSP13012543A ECSP13012543A EC SP13012543 A ECSP13012543 A EC SP13012543A EC SP13012543 A ECSP13012543 A EC SP13012543A EC SP13012543 A ECSP13012543 A EC SP13012543A
- Authority
- EC
- Ecuador
- Prior art keywords
- formula
- buprenorfine
- analogs
- compounds
- orl
- Prior art date
Links
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical class C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 title abstract 2
- 206010010774 Constipation Diseases 0.000 abstract 1
- 108090000137 Opioid Receptors Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 108010020615 nociceptin receptor Proteins 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
- C07D489/10—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
- C07D489/12—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención está dirigida a los compuestos análogos de Buprenorfina de la Fórmula I, Fórmula IA o Fórmula IB que se enseñan a continuación, en los cuales R1, R2, R8, R3a, R3b, G, X, Z e Y son como se han definido en la descripción. Los compuestos de la invención son útiles para tratar el dolor, la constipación, y otras condiciones moduladas por la actividad de los receptores opioide y ORL-1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38491210P | 2010-09-21 | 2010-09-21 | |
| US201161503674P | 2011-07-01 | 2011-07-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13012543A true ECSP13012543A (es) | 2013-06-28 |
Family
ID=44903285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13012543 ECSP13012543A (es) | 2010-09-21 | 2013-04-05 | Análogos de buprenorfina |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US9221831B2 (es) |
| EP (1) | EP2619212B1 (es) |
| JP (2) | JP5977240B2 (es) |
| KR (2) | KR101630912B1 (es) |
| CN (2) | CN103154000A (es) |
| AR (1) | AR083062A1 (es) |
| AU (1) | AU2011306644B2 (es) |
| CA (1) | CA2810356C (es) |
| CL (1) | CL2013000732A1 (es) |
| CO (1) | CO6690803A2 (es) |
| CR (1) | CR20130129A (es) |
| CY (1) | CY1117227T1 (es) |
| DK (1) | DK2619212T3 (es) |
| DO (1) | DOP2013000060A (es) |
| EA (1) | EA201390422A1 (es) |
| EC (1) | ECSP13012543A (es) |
| ES (1) | ES2566828T3 (es) |
| HR (1) | HRP20160281T1 (es) |
| HU (1) | HUE027195T2 (es) |
| ME (1) | ME02367B (es) |
| MX (1) | MX2013003354A (es) |
| NI (1) | NI201300032A (es) |
| NZ (1) | NZ609200A (es) |
| PE (1) | PE20140020A1 (es) |
| PH (1) | PH12013500530A1 (es) |
| PL (1) | PL2619212T3 (es) |
| RS (1) | RS54579B1 (es) |
| SG (1) | SG188300A1 (es) |
| SI (1) | SI2619212T1 (es) |
| SM (1) | SMT201600088B (es) |
| TW (2) | TW201242968A (es) |
| UY (1) | UY33618A (es) |
| WO (1) | WO2012038813A1 (es) |
| ZA (1) | ZA201301217B (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| JP2010531807A (ja) | 2007-05-25 | 2010-09-30 | トルマー セラピューティクス， インコーポレイテッド | リスペリドン化合物の徐放送達製剤 |
| GB2513060B (en) | 2010-06-08 | 2015-01-07 | Rb Pharmaceuticals Ltd | Microparticle buprenorphine suspension |
| US9272044B2 (en) | 2010-06-08 | 2016-03-01 | Indivior Uk Limited | Injectable flowable composition buprenorphine |
| JP6133772B2 (ja) | 2010-06-15 | 2017-05-24 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 痛み治療用の医薬配合物 |
| ES2648820T3 (es) | 2011-05-10 | 2018-01-08 | Gilead Sciences, Inc. | Compuestos heterocíclicos condensados como moduladores de los canales de sodio |
| NO3175985T3 (es) | 2011-07-01 | 2018-04-28 | ||
| TWI478908B (zh) | 2011-07-01 | 2015-04-01 | Gilead Sciences Inc | 作為離子通道調節劑之稠合雜環化合物 |
| WO2013084060A1 (en) | 2011-12-08 | 2013-06-13 | Purdue Pharma L.P. | Quaternized buprenorphine analogs |
| US9315514B2 (en) * | 2012-08-27 | 2016-04-19 | Rhodes Technologies | 1,3-dioxanomorphides and 1,3-dioxanocodides |
| EP3333156A3 (en) | 2012-11-09 | 2018-09-26 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US9175000B2 (en) | 2012-12-07 | 2015-11-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| US9056836B2 (en) | 2013-01-31 | 2015-06-16 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US8969358B2 (en) * | 2013-03-15 | 2015-03-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| EP3087079B1 (en) | 2013-12-26 | 2019-04-03 | Purdue Pharma LP | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
| EP3087073B1 (en) | 2013-12-26 | 2018-07-04 | Purdue Pharma LP | 10-substituted morphinan hydantoins |
| EP3087078B1 (en) | 2013-12-26 | 2019-05-15 | Purdue Pharma LP | 7-beta-alkyl analogs of orvinols |
| US20160333020A1 (en) * | 2013-12-26 | 2016-11-17 | Purdue Pharma L.P. | 7-beta analogs of orvinols |
| AU2014370062A1 (en) | 2013-12-26 | 2016-08-11 | Purdue Pharma L.P. | Ring-contracted morphinans and the use thereof |
| US10550088B2 (en) | 2013-12-27 | 2020-02-04 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
| GB201404139D0 (en) | 2014-03-10 | 2014-04-23 | Rb Pharmaceuticals Ltd | Sustained release buprenorphine solution formulations |
| JP2017521373A (ja) | 2014-05-27 | 2017-08-03 | パーデュー、ファーマ、リミテッド、パートナーシップ | スピロ環モルフィナン及びその使用 |
| EP3154972A4 (en) | 2014-06-13 | 2017-11-22 | Purdue Pharma L.P. | Azamophinan derivatives and use thereof |
| MA41125A (fr) | 2014-12-05 | 2017-10-10 | Purdue Pharma Lp | Dérivés de 6.7-cyclomorphinane et leur utilisation |
| AU2016344309A1 (en) * | 2015-10-26 | 2018-05-17 | Orphomed, Inc. | Ethylene glycol ether of buprenorphine |
| SI3390355T1 (sl) * | 2016-03-22 | 2023-07-31 | Helsinn Healthcare S. A. | Benzensulfonil-asimetrične sečnine in njihove medicinske uporabe |
| US10745402B2 (en) | 2017-01-02 | 2020-08-18 | Purdue Pharma L.P. | Morphinan derivatives and use thereof |
| EP3625235A1 (en) | 2017-05-19 | 2020-03-25 | River Stone Biotech, LLC | Preparation of buprenorphine |
| JP2021104932A (ja) * | 2018-03-30 | 2021-07-26 | 日本ケミファ株式会社 | モルヒナン誘導体の製造方法 |
| EP4577204A1 (en) * | 2022-08-23 | 2025-07-02 | Virginia Commonwealth University | Multiple targeting opioid receptor ligands as novel analgesics with minimum abuse liability |
| AU2024250576A1 (en) * | 2023-04-04 | 2025-11-13 | Board Of Regents, The University Of Texas System | METHODS OF SYNTHESIZING 14-β-AMINOMORPHANS AND SALTS THEREOF |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1136764A (en) * | 1965-08-13 | 1968-12-18 | Reckitt & Sons Ltd | Derivatives of thebaine and oripavine |
| AU732329B2 (en) | 1997-05-30 | 2001-04-12 | Banyu Pharmaceutical Co., Ltd. | 2-oxoimidazole derivative |
| TR200003598T2 (tr) | 1998-03-26 | 2001-06-21 | Japan Tobacco Inc. | Amid türevleri ve nosiseptin antagonistleri |
| NZ528241A (en) | 2001-03-02 | 2004-08-27 | Euro Celtique S | N-but-3-enyl norbuprenorphine and methods of use |
| US6740641B2 (en) | 2001-07-27 | 2004-05-25 | Euro-Celtique, S.A. | Sugar derivatives of hydromorphone, dihydromorphine and dihydromorphine, compositions thereof and uses for treating or preventing pain |
| KR20050074462A (ko) | 2002-09-25 | 2005-07-18 | 유로-셀티큐 에스.에이. | Ｎ―치환 하이드로모르폰 및 그 용도 |
| ATE444296T1 (de) | 2002-10-25 | 2009-10-15 | Euro Celtique Sa | Analoga und prodrugs von buprenorphin |
| US7202259B2 (en) | 2002-11-18 | 2007-04-10 | Euro-Celtique S.A. | Therapeutic agents useful for treating pain |
| US6958398B1 (en) | 2002-12-30 | 2005-10-25 | Euro-Celtique S.A. | Methods for making thebaine or its acid salts |
| ES2389456T3 (es) | 2006-11-01 | 2012-10-26 | Purdue Pharma Lp | Compuestos de fenilpropionamida y uso de los mismos |
| GB2447014A (en) * | 2007-03-01 | 2008-09-03 | Reckitt Benckiser Healthcare | Analgesic composition comprising a specific ratio of buprenorphine and naltrexone |
| AU2008331235C1 (en) | 2007-11-30 | 2013-01-17 | Purdue Pharma L.P. | Benzomorphan Compounds |
| CA2731939C (en) * | 2008-07-30 | 2017-05-23 | Purdue Pharma L.P. | Buprenorphine analogs |
| WO2013072758A1 (en) | 2011-11-15 | 2013-05-23 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| WO2013084060A1 (en) | 2011-12-08 | 2013-06-13 | Purdue Pharma L.P. | Quaternized buprenorphine analogs |
| US20150210646A1 (en) | 2012-05-11 | 2015-07-30 | Purdue Pharma L.P. | Benzomorphan compounds as opioid receptors modulators |
| US9315514B2 (en) | 2012-08-27 | 2016-04-19 | Rhodes Technologies | 1,3-dioxanomorphides and 1,3-dioxanocodides |
| EP3333156A3 (en) | 2012-11-09 | 2018-09-26 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US9175000B2 (en) | 2012-12-07 | 2015-11-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| WO2014091297A1 (en) | 2012-12-14 | 2014-06-19 | Purdue Pharma L.P. | Spirocyclic morphinans and their use |
| TWI513697B (zh) | 2012-12-14 | 2015-12-21 | Purdue Pharma Lp | 吡啶酮並嗎啡喃類似物及其對類鴉片受體之生物活性 |
| US8937084B2 (en) | 2012-12-14 | 2015-01-20 | Purdue Pharma L.P. | Nitrogen containing morphinan derivatives and the use thereof |
| US8957084B2 (en) | 2012-12-28 | 2015-02-17 | Purdue Pharma L.P. | 7,8-cyclicmorphinan analogs |
| US8946255B2 (en) | 2012-12-28 | 2015-02-03 | Purdue Pharma L.P. | Substituted morphinans and the use thereof |
| US9056836B2 (en) | 2013-01-31 | 2015-06-16 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US8969358B2 (en) | 2013-03-15 | 2015-03-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| EP3087073B1 (en) | 2013-12-26 | 2018-07-04 | Purdue Pharma LP | 10-substituted morphinan hydantoins |
| EP3087078B1 (en) | 2013-12-26 | 2019-05-15 | Purdue Pharma LP | 7-beta-alkyl analogs of orvinols |
| WO2015097546A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | Propellane-based compounds and their use as opioid receptor modulators |
| US20160333020A1 (en) | 2013-12-26 | 2016-11-17 | Purdue Pharma L.P. | 7-beta analogs of orvinols |
| US10550088B2 (en) | 2013-12-27 | 2020-02-04 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
| US9902726B2 (en) | 2013-12-30 | 2018-02-27 | Purdue Pharma L.P. | Pyridone-sulfone morphinan analogs as opioid receptor ligands |
-
2011
- 2011-09-20 MX MX2013003354A patent/MX2013003354A/es not_active Application Discontinuation
- 2011-09-20 WO PCT/IB2011/002208 patent/WO2012038813A1/en not_active Ceased
- 2011-09-20 HU HUE11776855A patent/HUE027195T2/en unknown
- 2011-09-20 HR HRP20160281TT patent/HRP20160281T1/hr unknown
- 2011-09-20 DK DK11776855.6T patent/DK2619212T3/en active
- 2011-09-20 PH PH1/2013/500530A patent/PH12013500530A1/en unknown
- 2011-09-20 ME MEP-2016-38A patent/ME02367B/me unknown
- 2011-09-20 KR KR1020137009943A patent/KR101630912B1/ko not_active Expired - Fee Related
- 2011-09-20 CA CA2810356A patent/CA2810356C/en not_active Expired - Fee Related
- 2011-09-20 NZ NZ609200A patent/NZ609200A/en not_active IP Right Cessation
- 2011-09-20 EA EA201390422A patent/EA201390422A1/ru unknown
- 2011-09-20 JP JP2013529723A patent/JP5977240B2/ja not_active Expired - Fee Related
- 2011-09-20 CN CN2011800450775A patent/CN103154000A/zh active Pending
- 2011-09-20 SI SI201130750T patent/SI2619212T1/sl unknown
- 2011-09-20 EP EP11776855.6A patent/EP2619212B1/en active Active
- 2011-09-20 UY UY0001033618A patent/UY33618A/es unknown
- 2011-09-20 SG SG2013014113A patent/SG188300A1/en unknown
- 2011-09-20 RS RS20160119A patent/RS54579B1/sr unknown
- 2011-09-20 AR ARP110103431A patent/AR083062A1/es unknown
- 2011-09-20 PL PL11776855.6T patent/PL2619212T3/pl unknown
- 2011-09-20 US US13/825,241 patent/US9221831B2/en active Active
- 2011-09-20 ES ES11776855.6T patent/ES2566828T3/es active Active
- 2011-09-20 PE PE2013000548A patent/PE20140020A1/es not_active Application Discontinuation
- 2011-09-20 AU AU2011306644A patent/AU2011306644B2/en not_active Ceased
- 2011-09-20 KR KR20157004529A patent/KR20150027315A/ko not_active Withdrawn
- 2011-09-20 CN CN201510733006.4A patent/CN105399751A/zh active Pending
- 2011-09-21 TW TW100133950A patent/TW201242968A/zh unknown
- 2011-09-21 TW TW102147960A patent/TW201422621A/zh unknown
-
2013
- 2013-02-18 ZA ZA2013/01217A patent/ZA201301217B/en unknown
- 2013-03-18 CL CL2013000732A patent/CL2013000732A1/es unknown
- 2013-03-20 DO DO2013000060A patent/DOP2013000060A/es unknown
- 2013-03-20 NI NI201300032A patent/NI201300032A/es unknown
- 2013-03-21 CR CR20130129A patent/CR20130129A/es not_active Application Discontinuation
- 2013-04-05 EC ECSP13012543 patent/ECSP13012543A/es unknown
- 2013-04-18 CO CO13100225A patent/CO6690803A2/es unknown
-
2015
- 2015-11-19 JP JP2015226945A patent/JP2016102115A/ja not_active Withdrawn
-
2016
- 2016-03-04 CY CY20161100187T patent/CY1117227T1/el unknown
- 2016-03-24 SM SM201600088T patent/SMT201600088B/xx unknown
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